MK-1439 (ID: DG01286) Resistance Data of HIV

Drug Resistance Data Categorized by Their Corresponding Mechanisms
Aberration of the Drug's Therapeutic Target (ADTT)			Click to Show/Hide
Key Molecule: HIV1 Reverse transcriptase (HIV1 RT)				Molecule Info
Resistant Disease	Human immunodeficiency virus infection [ICD-11: 1C62.0]
Molecule Alteration	Alteration Patterns Alteration Types Resistance Mutation Total Point Scores Levels of Drug resistance base on the total point score Ref p.Y188L Missense mutation N.A. Resistance [1]
Resistant Drug	MK-1439			Drug Info
Experimental Note	Identified from the Human Clinical Data
In Vitro Model	AIP KO MEF cells	Skin	Mus musculus (Mouse)	CVCL_UJ02
	MT4 cells	Umbilical cord blood	Homo sapiens (Human)	CVCL_2632
Experiment for Molecule Alteration	PCR
Mechanism Description	The cyanochlorophenol moiety forms pai-pai stacking with Y188, and the Y188L substitution eliminates the pai-pai interactions and creates a clash with DOR; thus, the Y188L substitution confers significant resistance to DOR, suggesting that the pai-pai interactions between the residues are crucial for the binding of DOR to RT.

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